The present invention relates to novel isoquinolinone and isothiochromone compounds that possess anti-allergy activity.
British Patent 047485 discloses compounds of the general formula ##STR2## wherein: X is 0, S or NH;
R is H or alkyl; and PA1 R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each is chosen from H, halogen, alkyl, alkoxy, aryl, aralkyl, acyloxy, heterocyclic or CO.sub.2 H. These compounds are disclosed as having anti-allergy activity, inhibiting known antigen-antibody reactions and being useful in the prophylaxis and therapy of diseases caused by allergic or immunological reactions. PA1 R.sup.1 is H or CH.sub.3 ; PA1 R.sup.2 is H or OCH.sub.3 ; and PA1 R.sup.3 is H or CH.sub.3. PA1 1,2,3,4-tetrahydro-8,10-dihydroxy-11-6H-benzo[b]quinolizin-6-one, PA1 1,2,3,4-tetrahydro-8,10,11-trihydroxy-6H-benzo[b]quinolizin-6-one, PA1 5,7-dihydroxy-4-phenyl-1(2H)-dihydroisoquinolinone, PA1 1,2,3,4-tetrahydro-9,10-dihydroxy-11-methyl-6H-benzo[b]quinolizin-6-one, PA1 1,3,4,5-tetrahydro-8,10-dihydroxy-phenanthridin-6(2H)-one, PA1 1,2,3,4,11,11a-hexahydro-8,10,11-trihydroxy-11-phenyl-6H-benzo[b]quinolizin -6-one, PA1 2,3-dihydro-7,9-dihydroxy-10-phenylpyrrolo[1,2-b]isoquinolin-5(1H)-one, PA1 9,10-bis(acetyloxy)-1,2,3,4,11,11a-hexahydro-11-methylene-6H-benzo[b]quinol izin-6-one, PA1 8,10-bis(acetyloxy)-1,2,3,4,-tetrahydro-11-phenyl-6H-benzo[b]quinolizin-6-o ne, PA1 8,10,11-tris(acetyloxy)-1,2,3,4-tetrahydro-6H-benzo[b]quinolizin-6-one, PA1 8,10-bis(2,2-dimethyl-1-oxopropoxy)-11-methyl-1,3,4,6-tetrahydro-6H-benzo[b ]quinolizin-6-one, PA1 7,8-bis(acetyloxy)-1,2,3,4-tetrahydro-11-methyl-6H-benzo[b]quinolizin-6-one PA1 8-acetyloxy-1,2,3,4-tetrahydro-11-methyl-6H-benzo[b]quinolizin-6-one, PA1 9,10-bis(acetyloxy)-1,2,3,4-tetrahydro-11-methyl-6H-benzo[b],-QUINOLIZIN-6- one, PA1 7,9-bis(acetyloxy)-2,3-dihydro-10-methyl-pyrrolo[1,2-b]isoquinolin-5(1H)-on e, PA1 5,7-bis(acetyloxy)-4-methyl-1(2H)-isoquinolinone, PA1 5,7-bis(acetyloxy)-4-phenyl-1(2H)-isoquinolinone, PA1 5,7-bis(acetyloxy)-3-methyl-4-phenyl-1(2H)-isoquinolinone, PA1 5,7-bis(acetyloxy)-2,3-dimethyl-4-phenyl-1(2H)-iso-quinolinone, PA1 8,10-bis(acetyloxy)-1,3,4,5,6-tetrahydro-6(2H)-phenanthridinone, PA1 8,10-bis(acetyloxy)-1,2,3,4-tetrahydro-11-methyl-6H-benzo[b]quinolizin-6-on e, PA1 7,9-bis(acetyloxy)-2,3-dihydro-10-phenyl-6H-pyrrolo[1,2-b]isoquinolin-5(1H) -one, PA1 8-acetyloxy-1,2,3,4,11,11a-hexahydro-11-hydroxy-11-methyl-6H-benzo[b]quinol izin-6-one, PA1 1,2,3,4-tetrahydro-8,10-dihydroxy-11-methyl-6H-benzo[b]quinolizin-6-one, disodium salt PA1 8,10-bis[(aminoacetyl)oxy]-11-methyl-1,2,3,4-tetrahydro-6H-benzo[b]quinoliz ine-6-one, PA1 8,10-bis[(aminoacetyl)oxy]-11-methyl-1,2,3,4-tetrahydro-6H-benzo[b]quinoliz ine-6-one dihydrochloride, PA1 5,7-bis(acetyloxy)-2,3-dimethyl-4-phenyl-1(2H)isoquinolin-1-one, PA1 8,10-bis(acetyloxy)-1,3,4,5-tetrahydro-5-methyl-6(2H)-phenanthridinone, PA1 8,10-bis(methoxy)-1,2,3,4-tetrahydro-11-methyl-6H-benzo[b]quinolizin-6-one, or PA1 1,2,3,4-tetrahydro-8,10-dihydroxy-6H-benzo[b]quinolizin-6-one.
Coppola, J. Heterocyclic Chem. 1981 18, 767, discloses compounds of the general formula ##STR3## wherein n can be 1, 2 or 3. No activities for these compounds are disclosed or discussed.
Shiraiwa et al., Chem. Pharm. Bull. 1983, 31, 2275, discloses compounds of general formulas ##STR4## wherein X is Br or OH. No activities for these compounds are disclosed or discussed.
Chem. Absts. 1965, 62, 16179e, discloses compounds of the general formula ##STR5## wherein R is H, OH or OCH.sub.3 ;
No activities for these compounds are disclosed or discussed.